The ability to effectively treat bacterial infectious diseases through the use of antimicrobial chemotherapy has been severely affected by the widespread emergence of antibiotic resistance among bacterial pathogens. Examples of multi-drug resistant bacterial strains that have emerged include Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Mycobacterium tuberculosis, Enterococcus faecalis, Proprionibacterium acnes, and Escherichia coli. These antibiotic resistant bacteria present serious health care concerns worldwide and, in fact, antibiotic resistant bacteria are a major cause of morbidity and mortality in both hospital and community settings. There is therefore an urgent need to combat this problem effectively.
One approach to combating antibiotic resistance is to develop novel classes of compounds that exhibits good antibacterial activity and are applicable for the treatment and/or prophylactic management of bacterial infections. Naturally occurring tetramic acid derivatives are a great deal of interest because of their broad spectrum of antibacterial activity. Examples of naturally occurring tetramic acid derivates that exhibit antibacterial activity include reutericyclin, streptolydigin, PF1052, and erythroskyrine. No tetramic acid derivative antibiotics are marketed at present.
A significant need exists for tetramic acid derivatives having antibacterial activity which derivatives are can be produced synthetically.